Luteolin from Flos Chrysanthemi and its derivatives: New small molecule Bcl-2 protein inhibitors.
Bioorg Med Chem Lett
; 24(19): 4672-4677, 2014 Oct 01.
Article
em En
| MEDLINE
| ID: mdl-25193233
ABSTRACT
Over-expression of the Bcl-2 anti-apoptotic proteins is closely related to tumorigenesis and associated with drug resistance. Here we report that luteolin, a main substance found in Flos Chrysanthemi, directly binds to and shows inhibitory activity against the Bcl-2 protein. We studied the binding mode of luteolin and its derivatives with target proteins, their structure-activity relationship, and their effect on the human leukemia cell line HL-60. The results suggest that luteolin and its derivatives with a benzyl group introduced to the B ring, are new small molecule Bcl-2 protein inhibitors, and their anti-tumor activity is likely related to their effect on the Bcl-2 protein.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Proteínas Proto-Oncogênicas c-bcl-2
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Chrysanthemum
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Flores
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Luteolina
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Bibliotecas de Moléculas Pequenas
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Antineoplásicos Fitogênicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article